Synthetic methodologies for the construction of novel nucleoside derivatives with potential antiviral and anticancer activity

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Nucleosides and nucleotides are essential biomolecules for the functioning of cellular systems in all living organisms. Both nucleosides and nucleotides have been developed as drug molecules, but nucleosides possess enhanced physicochemical properties that allow them to penetrate cell membranes. Moreover, nucleosides are readily converted into active nucleotides via cellular phosphorylation processes, such as cell signaling, DNA and RNA synthesis, enzyme regulation and metabolism. Therefore, new and improved synthetic routes for nucleosides are of considerable interest in drug discovery programs of and will benefit many Canadian and international pharmaceutical companies. This research proposal aims to develop efficient synthetic methods for the preparation of nucleoside analogues bearing original features such as: a) introduction of functional groups at the 1' position and b) conformational restriction of the sugar backbone. The introduction of these structural elements will provide opportunities for novel interactions with biological targets of interest in the fields of anticancer and antiviral drug discovery. By targeting such nucleosides, this collaboration will lead to low-cost and locally produced medicines for Canadians, all while aiding to develop young scientific minds that would otherwise not have the opportunity to participate in high-impact industrial collaborations at the undergraduate level.